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噻唑烷-2,4-二酮共轭物作为PPAR-γ激动剂的设计、合成及生物学评价

Design, Synthesis, and Biological Evaluation of Thiazolidine-2,4-dione Conjugates as PPAR-γ Agonists.

作者信息

Nazreen Syed, Alam Mohammad Sarwar, Hamid Hinna, Shahar Yar Mohammad, Dhulap Abhijeet, Alam Perwez, Pasha Mohammad Abdul Qadar, Bano Sameena, Alam Mohammad Mahboob, Haider Saqlain, Kharbanda Chetna, Ali Yakub, Pillai Kolakappi

机构信息

Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi, India.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi, India.

出版信息

Arch Pharm (Weinheim). 2015 Jun;348(6):421-32. doi: 10.1002/ardp.201400280. Epub 2015 Apr 21.

DOI:10.1002/ardp.201400280
PMID:25900064
Abstract

A library of synthesized conjugates of phenoxy acetic acid and thiazolidinedione 5a-m showed potent peroxisome proliferator activated receptor-γ (PPAR-γ) transactivation as well as significant blood glucose lowering effect comparable to the standard drugs pioglitazone and rosiglitazone. Most of the compounds showed higher docking scores than the standard drug rosiglitazone in the molecular docking study. Compounds 5l and 5m exhibited PPAR-γ transactivation of 54.21 and 55.41%, respectively, in comparison to the standard drugs pioglitazone and rosiglitazone, which showed 65.94 and 82.21% activation, respectively. Compounds 5l and 5m significantly lowered the blood glucose level of STZ-induced diabetic rats. Compounds 5l and 5m lowered the AST, ALT, and ALP levels more than the standard drug pioglitazone. PPAR-γ gene expression was significantly increased by compound 5m (2.00-fold) in comparison to the standard drugs pioglitazone (1.5-fold) and rosiglitazone (1.0-fold). Compounds 5l and 5m did not cause any damage to the liver and could be considered as promising candidates for the development of new antidiabetic agents.

摘要

苯氧乙酸与噻唑烷二酮5a - m的合成共轭物库显示出强大的过氧化物酶体增殖物激活受体-γ（PPAR - γ）反式激活作用，以及与标准药物吡格列酮和罗格列酮相当的显著降血糖效果。在分子对接研究中，大多数化合物的对接分数高于标准药物罗格列酮。与分别显示65.94%和82.21%激活率的标准药物吡格列酮和罗格列酮相比，化合物5l和5m的PPAR - γ反式激活率分别为54.21%和55.41%。化合物5l和5m显著降低了链脲佐菌素诱导的糖尿病大鼠的血糖水平。化合物5l和5m降低天冬氨酸转氨酶（AST）、丙氨酸转氨酶（ALT）和碱性磷酸酶（ALP）水平的效果优于标准药物吡格列酮。与标准药物吡格列酮（1.5倍）和罗格列酮（1.0倍）相比，化合物5m使PPAR - γ基因表达显著增加（2.00倍）。化合物5l和5m对肝脏未造成任何损伤，可被视为开发新型抗糖尿病药物的有前景的候选物。

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引用本文的文献

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